Oral bioavailability of ketoprofen in suspension and solution formulations in rats: the influence of poloxamer 188.
J Pharm Pharmacol
; 64(11): 1631-7, 2012 Nov.
Article
in En
| MEDLINE
| ID: mdl-23058050
ABSTRACT
OBJECTIVES:
The aim of the current study was to investigate the effect of poloxamer 188 (P-188) on the bioavailability of the BCS class 2 drug ketoprofen in vivo.METHODS:
Aqueous suspension and solution formulations of ketoprofen with and without P-188 were orally administered to fasted male Wistar rats. The intrinsic dissolution rate and solubility of ketoprofen in simulated intestinal fluid, in both the presence and absence of P-188, was measured. KEYFINDINGS:
The AUC and C(max) were found to be significantly enhanced when ketoprofen was administered as suspension and P-188 was present in the formulation (Susp P-188) as compared to the surfactant-free formulation (â¼4-fold higher AUC, 7-fold higher C(max) ). While drug solubility appeared to be almost unaffected by P-188, a significantly faster dissolution was observed. In addition, the influence of P-188 on the drug absorption process was investigated by comparison of solution formulations with and without P-188.CONCLUSIONS:
The in-vivo performance of these solutions, a pure buffer solution and a P-188-containing buffer solution showed no significant difference, suggesting that the increase in bioavailability for Susp P-188 was primarily a consequence of the dissolution rate-enhancing effect.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Anti-Inflammatory Agents, Non-Steroidal
/
Ketoprofen
/
Poloxamer
/
Excipients
Type of study:
Prognostic_studies
Limits:
Animals
/
Humans
/
Male
Language:
En
Journal:
J Pharm Pharmacol
Year:
2012
Document type:
Article
Affiliation country:
Denmark